Formulation and in vivo human bioavailability of dissolving tablets containing a self-nanoemulsifying itraconazole solid dispersion without precipitation in simulated gastrointestinal fluid

摘要

Solid dispersion (SD), which is defined as the dispersion of one or more active ingredients in an inert hydrophilic carrier or matrix, is commonly used to improve the dissolution rate of various poorly water-soluble drugs because of its simplicity and ease of manufac-turability (Heo et al., 2005; Park et al., 2007). However, conventional SD requires various pharmaceutical excipients, such as solubilisers, surfactants, oils and fatty acids, or mixtures of these aforementioned excipients to overcome the limited solubilising enhancement of SD alone (Heo et al., 2005; Shim et al., 2006; Park et al., 2007). In contrast, self-emulsifying or self-microemulsifying drug delivery systems can also be successfully used to improve the oral bioavailability of poorly water-soluble drugs and are normally prepared as liquids (Attama et al., 2003; Franceschinisa et al., 2005; Shim et al., 2006; Park et al., 2007; Woo et al., 2008).